EEDi-5285 是一种非常有效且具有口服活性的胚胎外胚层发育 (EED) 抑制剂，结合 EED 蛋白的 IC₅₀ 值为 0.2 nM，并具有抗癌活性。

EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC 50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity.

Solid

IC50: 0.2 nM (Embryonic ectoderm development (EED))

EEDi-5285 inhibits cell growth with IC50 values of 20 pM and 0.5 nM in the Pfeiffer and KARPAS422 lymphoma cell lines, respectively, carrying an EZH2 mutation. has not independently confirmed the accuracy of these methods. They are for reference only.

EEDi-5285 (compound 28; 50-100 mg/kg; oral gavage; daily; for 28 days; SCID mice) treatment achieves complete and durable tumor regression in the KARPAS422 xenograft model in mice with oral administration.
A single 100 mg/kg oral administration of EEDi-5285 (compound 28) effectively reduces the level of H3K27me3 at 24 h in KARPAS422 tumor tissue in mice.
EEDi-5285 (compound 28) achieves a C max of 1.8 μM and an AUC of 6.0 h?μg/ml with 10 mg/kg oral administration and has an oral bioavailability (F) of 75%. EEDi-5285 has a moderate volume of distribution of 1.4 L/kg and a terminal T 1/2 of approximately 2 h. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；In solvent -80°C 6 months

[1]. Rohan Kalyan Rej, et al. EEDi-5285: An Exceptionally Potent, Efficacious, and Orally Active Small-Molecule Inhibitor of Embryonic Ectoderm Development. J Med Chem. 2020 Jul 9;63(13):7252-7267.

In Vitro: DMSO : 125 mg/mL (260.67 mM; Need ultrasonic)配制储备液